Claims for Patent: 8,026,238

Summary for Patent: 8,026,238

Title:	Topical antifungal composition
Abstract:	A topical, foamable composition is provided that includes at least one antifungal agent that is able to penetrate the upper layers of skin and is retained in or on an area to be treated for a prolonged period of time, and that has a residual non-volatile component content of less than 25%. In addition, a method of treating fungal diseases including jock itch, tinea, dandruff and sebborheic dermatitis is provided, and includes applying to the affected area of a patient requiring such treatment an antifungal composition.
Inventor(s):	Davey; Greg (Rowville, AU), Abram; Albert Zorko (Rowville, AU)
Assignee:	Stiefel Research Australia, Pty Ltd (Rowville, Victoria, AU)
Application Number:	12/293,000
Patent Claims:	1. A method for treating fungal diseases, comprising: (a) providing a topical, foamable composition which in use produces a temperature sensitive, quick-breaking foam or mousse, the composition consisting essentially of: one or more antifungal agents selected from the group consisting of an imidazole compound and a triazole compound, wherein the antifungal agent is capable of penetrating the upper layers of skin of a user, at least one surfactant, water, a lower alcohol, a long chain alcohol, a residual non-volatile component content of less than 25% by weight, and a hydrocarbon gas propellant content of less than 60% by weight; wherein the one or more antifungal agents is dissolved in the lower alcohol; and (b) applying the topical, foamable composition to user's skin, whereupon the antifungal agent is retained in or on skin for a period of time sufficient to achieve skin penetration. 2. The method of claim 1, wherein the lower alcohol is ethanol with a content of greater than 50% by weight. 3. The method of claim 1, wherein the content of the residual non-volatile component is less than 10% by weight. 4. The method of claim 1, wherein the provided topical foamable composition consists essentially of: up to 5% by weight of long chain alcohol; up to 10% by weight of propylene glycol; up to 5% by weight of the antifungal agent; up to 90% by weight of lower alcohol; up to 5% by weight of surfactant; 5-95% by weight of water; and up to 20% by weight of the hydrocarbon gas propellant. 5. The method of claim 1, wherein the antifungal agent is ketoconazole. 6. The method of claim 1, wherein the surfactant is selected from the group consisting of a quaternary compound, ethoxylated sorbitan esters, ethoxylated sorbitan palmitate, ethoxylated sorbitan oleate, a nonyl phenol ethoxylated and a fatty alcohol ethoxylate, and mixtures thereof. 7. A topical, foamable composition, consisting essentially of: (a) one or more antifungal agents selected from the group consisting of an imidazole compound and a triazole compound; (b) at least one surfactant; (c) a lower alcohol content of greater than 50% by weight; (d) water; (e) a long chain alcohol; (f) a residual non-volatile component content of less than 25% by weight; and (g) a propellant; wherein the one or more antifungal agents is dissolved in the ethanol; and wherein the composition produces a temperature-sensitive, quick-breaking foam or mousse when used. 8. The composition of claim 7, wherein the content of the residual non-volatile component is less than 10% by weight. 9. The composition of claim 7, wherein the composition is a mousse. 10. The composition of claim 9, wherein the propellant is a hydrocarbon gas propellant in an amount of less than 60% by weight. 11. The composition of claim 7, wherein the lower alcohol is ethanol. 12. The composition of claim 7, consisting essentially of: up to 5% by weight of long chain alcohol; up to 10% by weight of propylene glycol; up to 5% by weight of the antifungal agent; up to 90% by weight of lower alcohol; up to 5% by weight of surfactant; 5-95% by weight of water; and up to 20% by weight of hydrocarbon gas propellant. 13. The composition of claim 7, wherein the antifungal agent is ketoconazole. 14. The composition of claim 7, wherein the surfactant is selected from the group consisting of a quaternary compound, ethoxylated sorbitan stearate, ethoxylated sorbitan palmitate, ethoxylated sorbitan oleate, a nonyl phenol ethoxylate and a fatty alcohol ethoxylate, and mixtures thereof. 15. A topical, foamable composition, consisting essentially of: (a) one or more antifungal agents in an amount of up to 5% by weight, the one or more antifungal agents being selected from the group consisting of an imidazole compound and a triazole compound, wherein the antifungal agent is capable of penetrating the upper layers of skin of a user; (b) a lower alcohol content of greater than 50% by weight and up to 90% by weight, wherein the lower alcohol is ethanol; (c) at least one surfactant in an amount of up to 5% by weight; (d) up to 5% by weight of a long chain alcohol or mixtures thereof; (e) up to 10% by weight propylene glycol; and (f) 5-95% by weight water; wherein the antifungal agent is retained in or on skin for a period of time sufficient to penetrate the epidermis of a user. 16. The topical, foamable composition of claim 15, wherein the imidazole compound is ketoconazole. 17. The topical, foamable composition of claim 15, wherein the surfactant is polyoxyethylene sorbitan monostearate. 18. The topical, foamable composition of claim 15, wherein the long chain alcohol is selected from the group consisting of cetyl alcohol, stearyl alcohol, and mixtures thereof. 19. A topical, foamable composition, consisting essentially of: (a) one or more antifungal agents in an amount of up to 5% by weight, the one or more antifungal agents being selected from the group consisting of an imidazole compound and a triazole compound; (b) ethanol at greater than 50% by weight and up to 90% by weight; (c) polyoxyethylene sorbitan monostearate in an amount of up to 5% by weight; (d) up to 5% by weight cetyl alcohol or stearyl alcohol or mixtures thereof; (e) up to 10% by weight propylene glycol; and (f) 5-95% by weight water; wherein the antifungal agent is retained in or on skin for a period of time sufficient to penetrate the epidermis of a user. 20. The topical, foamable composition of claim 19, wherein the imidazole compound is ketoconazole. 21. A method for treating fungal diseases, comprising: (a) providing a topical, foamable composition consisting essentially of one or more antifungal agents selected from the group consisting of an imidazole compound and a triazole compound, wherein the antifungal agent is capable of penetrating the upper layers of skin of a user, at least one surfactant, water, a lower alcohol content of greater than 10% by weight, a long chain alcohol, and hydrocarbon gas propellant in an amount of less than 60% by weight of the total composition, wherein the composition is a temperature sensitive quick breaking foam or mousse and has a residual non-volatile component content of less than 25% by weight; and (b) applying the topical, foamable composition to user's skin, whereupon the antifungal agent is retained in or on skin for a period of time sufficient to achieve skin penetration. 22. The method of claim 21, wherein the content of the residual non-volatile component is less than 10% by weight. 23. The method of claim 22, wherein the content of the residual non-volatile component is less than 6% by weight. 24. The method of claim 21, wherein the composition has a hydrocarbon gas propellant content of less than 10% by weight. 25. The method of claim 21, wherein the provided topical, foamable composition consists essentially of: up to 5% by weight of long chain alcohol; up to 10% by weight of propylene glycol; up to 5% by weight of the antifungal agent; up to 90% by weight of lower alcohol; up to 5% by weight of surfactant; 5-95% by weight of water; and up to 20% by weight of a hydrocarbon gas propellant. 26. The method of claim 21, wherein the lower alcohol content is greater than 50% by weight. 27. The method of claim 21, wherein the lower alcohol is ethanol. 28. The method of claim 21, wherein the lower alcohol and water are present in a ratio of about 1.65 to about 1 by weight. 29. The method of claim 21, wherein the long chain alcohol is selected from the group consisting of cetyl alcohol, stearyl alcohol, and mixtures thereof. 30. The method of claim 21, wherein the antifungal agent is ketoconazole. 31. The method of claim 21, wherein the surfactant is selected from the group consisting of a quaternary compound, ethoxylated sorbitan stearate, ethoxylated sorbitan palmitate, ethoxylated sorbitan oleate, a nonyl phenol ethoxylate and a fatty alcohol ethoxylate, and mixtures thereof. 32. A topical, foamable composition consisting essentially of: (a) one or more antifungal agents selected from the group consisting of an imidazole compound and a triazole compound; (b) at least one surfactant; (c) a lower alcohol content of greater than 10% by weight; (d) water; (e) a long chain alcohol; (f) hydrocarbon gas propellant in an amount of less than 60% by weight; and wherein the composition is a temperature-sensitive, quick-breaking foam or mousse, and wherein the composition contains a residual non-volatile component content in an amount of less than 25% by weight. 33. The composition of claim 32, wherein the content of the residual non-volatile component is less than 10% by weight. 34. The composition of claim 33, wherein the content of the residual non-volatile component is less than 6% by weight. 35. The composition of claim 32, wherein the hydrocarbon gas propellant is present in an amount of less than 10% by weight. 36. The composition of claim 32, consisting essentially of: up to 5% by weight of long chain alcohol; up to 10% by weight of propylene glycol; up to 5% by weight of the antifungal agent; up to 90% by weight of lower alcohol; up to 5% by weight of surfactant; 5-95% by weight of water; and up to 20% by weight of a hydrocarbon gas propellant. 37. The composition of claim 32, wherein the lower alcohol content is greater than 50% by weight. 38. The composition of claim 32, wherein the lower alcohol is ethanol. 39. The composition of claim 32, wherein the lower alcohol and water are present in a ratio of about 1.65 to about 1 by weight. 40. The composition of claim 32, wherein the long chain alcohol is selected from the group consisting of cetyl alcohol, stearyl alcohol, and mixtures thereof. 41. The composition of claim 32, wherein the antifungal agent is ketoconazole. 42. The composition of claim 32, wherein the surfactant is selected from the group consisting of a quaternary compound, ethoxylated sorbitan stearate, ethoxylated sorbitan palmitate, ethoxylated sorbitan oleate, a nonyl phenol ethoxylate and a fatty alcohol ethoxylate and mixtures thereof. 43. A topical, foamable composition consisting essentially of: (a) one or more antifungal agents in an amount of up to 5% by weight, the one or more antifungal agents being selected from the group consisting of an imidazole compound and a triazole compound, wherein the antifungal agent is capable of penetrating the upper layers of skin of a user; (b) a lower alcohol content of greater than 50% by weight and up to 90% by weight, wherein the lower alcohol is ethanol; (c) at least one surfactant in an amount of up to 5% by weight; (d) up to 5% by weight of a long chain alcohol or mixtures thereof; (e) up to 10% by weight propylene glycol; (f) 5-34% by weight water; and (g) less than 10% by weight hydrocarbon gas propellant; wherein the antifungal agent is retained in or on skin for a period of time sufficient to penetrate the epidermis of a user. 44. The topical, foamable composition of claim 43, wherein the imidazole compound is ketoconazole. 45. The topical, foamable composition of claim 43, wherein the surfactant is polyoxyethylene sorbitan monostearate. 46. The topical, foamable composition of claim 43, wherein the long chain alcohol is selected from the group consisting of cetyl alcohol, stearyl alcohol, and mixtures thereof. 47. A topical, foamable composition consisting essentially of: (a) one or more antifungal agents in an amount of up to 5% by weight, the one or more antifungal agents being selected from the group consisting of an imidazole compound and a triazole compound; (b) ethanol at greater than 50% by weight and up to 90% by weight; (c) polyoxyethylene sorbitan monostearate in an amount of up to 5% by weight; (d) up to 5% by weight cetyl alcohol or stearyl alcohol or mixtures thereof; (e) up to 10% by weight propylene glycol; (f) 5 to about 34% by weight water; and (g) less than 10% by weight hydrocarbon gas propellant; wherein the antifungal agent is retained in or on skin for a period of time sufficient to penetrate the epidermis of a user. 48. The topical, foamable composition of claim 47, wherein the imidazole compound is ketoconazole. 49. A method for treating fungal diseases, comprising: (a) providing a topical, foamable composition which in use produces a temperature-sensitive, quick-breaking foam or mousse, the composition consisting essentially of: one or more antifungal agents selected from the group consisting of an imidazole compound and a triazole compound, wherein the antifungal agent is capable of penetrating the upper layers of skin of a user, at least one surfactant selected from the group consisting of a quaternary compound, ethoxylated sorbitan stearate, ethoxylated sorbitan palmitate, ethoxylated sorbitan oleate, a nonyl phenol ethoxylate and a fatty alcohol ethoxylate, and mixtures thereof, water, a lower alcohol, a long chain alcohol, and a residual non-volatile component content of less than 25% by weight; wherein the lower alcohol is ethanol with a content of greater than 50% by weight and the one or more antifungal agents is dissolved in the ethanol; and (b) applying the topical, foamable composition to user's skin, whereupon the antifungal agent is retained in or on skin for a period of time sufficient to achieve skin penetration. 50. A topical, foamable composition, consisting essentially of: (a) one or more antifungal agents selected from the group consisting of an imidazole compound and a triazole compound; (b) at least one surfactant selected from the group consisting of a quaternary compound, ethoxylated sorbitan stearate, ethoxylated sorbitan palm itate, ethoxylated sorbitan oleate, a nonyl phenol ethoxylate and a fatty alcohol ethoxylate, and mixtures thereof; (c) an ethanol content of greater than 50% by weight; (d) water; (e) a long chain alcohol; (f) a residual non-volatile component content of less than 25% by weight, wherein the one or more antifungal agents is dissolved in the ethanol; and wherein the composition produces a temperature-sensitive, quick-breaking foam or mousse when used. 51. A topical, foamable composition, consisting essentially of: (a) one or more antifungal agents in an amount of up to 5% by weight, the one or more antifungal agents being selected from the group consisting of an imidazole compound and a triazole compound, wherein the antifungal agent is capable of penetrating the upper layers of skin of a user; (b) a lower alcohol content of greater than 50% by weight and up to 90% by weight, wherein the lower alcohol is ethanol; (c) at least one surfactant in an amount of up to 5% by weight, the at least one surfactant being selected from the group consisting of a quaternary compound, ethoxylated sorbitan stearate, ethoxylated sorbitan palmitate, ethoxylated sorbitan oleate, a nonyl phenol ethoxylate and a fatty alcohol ethoxylate, and mixtures thereof; (d) up to 5% by weight of a long chain alcohol or mixtures thereof; (e) up to 10% by weight propylene glycol; and (f) 5-95% by weight water; wherein the antifungal agent is retained in or on skin for a period of time sufficient to penetrate the epidermis of a user. 52. A method for treating fungal diseases, comprising: (a) providing a topical, foamable composition consisting essentially of one or more antifungal agents selected from the group consisting of an imidazole compound and a triazole compound, wherein the antifungal agent is capable of penetrating the upper layers of skin of a user, at least one surfactant selected from the group consisting of a quaternary compound, ethoxylated sorbitan stearate, ethoxylated sorbitan palmitate, ethoxylated sorbitan oleate, a nonyl phenol ethoxylate and a fatty alcohol ethoxylate, and mixtures thereof, water, a lower alcohol content of greater than 10% by weight, a long chain alcohol, and hydrocarbon gas propellant in an amount of less than 60% by weight of the total composition, wherein the composition is a temperature sensitive quick breaking foam or mousse and has a residual non-volatile component content of less than 25% by weight; and (b) applying the topical, foamable composition to user's skin, whereupon the antifungal agent is retained in or on skin for a period of time sufficient to achieve skin penetration. 53. A topical, foamable composition consisting essentially of: (a) one or more antifungal agents selected from the group consisting of an imidazole compound and a triazole compound; (b) at least one surfactant selected from the group consisting of a quaternary compound, ethoxylated sorbitan stearate, ethoxylated sorbitan palmitate, ethoxylated sorbitan oleate, a nonyl phenol ethoxylate and a fatty alcohol ethoxylate, and mixtures thereof; (c) a lower alcohol content of greater than 10% by weight; (d) water; (e) a long chain alcohol; (f) hydrocarbon gas propellant in an amount of less than 60% by weight; and wherein the composition is a temperature-sensitive, quick-breaking foam or mousse, and has a residual non-volatile component content of less than 25% by weight. 54. A topical, foamable composition consisting essentially of: (a) one or more antifungal agents in an amount of up to 5% by weight, the one or more antifungal agents being selected from the group consisting of an imidazole compound and a triazole compound, wherein the antifungal agent is capable of penetrating the upper layers of skin of a user; (b) a lower alcohol content of greater than 50% by weight and up to 90% by weight, wherein the lower alcohol is ethanol; (c) at least one surfactant in an amount of up to 5% by weight, the at least one surfactant being selected from the group consisting of a quaternary compound, ethoxylated sorbitan stearate, ethoxylated sorbitan palmitate, ethoxylated sorbitan oleate, a nonyl phenol ethoxylate and a fatty alcohol ethoxylate, and mixtures thereof; (d) up to 5% by weight of a long chain alcohol or mixtures thereof; (e) up to 10% by weight propylene glycol; (f) 5-34% by weight water; and (g) less than 10% by weight hydrocarbon gas propellant; wherein the antifungal agent is retained in or on skin for a period of time sufficient to penetrate the epidermis of a user.